As one of the natural flavonoids, diosmin has a strong antioxidant effect. Zou Shujun and others proved that diosmin has a certain scavenging effect on DPPH· and O2. And with the increase of the concentration, the clearance rate showed an upward trend, that is, there was a dose-effect relationship. Comparing the change of absorbance value at 517 nm wavelength of 95% ethanol solution containing 1,1-diphenyl-2-trinitrophenylhydrazine radical (DPPH·) before and after adding diosmin, it was found that after adding diosmin, The absorbance value of the solution decreases, indicating that the single-electron pairing of diosmin and DPPH· reduces the concentration of DPPH· in the solution, which proves that diosminin has the ability to scavenge DPPH·free radicals, and has strong antioxidant activity, and its activity is stronger than that of VitC .
Globally, the increasing number of methicillin-resistant Staphylococcus aureus (MRSA) has limited treatment options, and natural compounds have been shown to be antimicrobial against MRSA. Geranolin has no direct antibacterial activity against MRSA strains, however, geranolin significantly inhibits the activity of MRSA pyruvate kinase in a dose-dependent manner, which may lead to the lack of ATP, affecting the bacterial jet pump, and making geranolin inhibit the activity of MRSA pyruvate kinase. MRSA is bacteriostatic.
In the human breast epithelial carcinoma cell line MCF-7, diosmin treatment increased the activity of cytochrome P450 1A1 (CYP1A1) in a dose- and time-dependent manner. By increasing the level of CYP1A1 mRNA, diosmin increased the transcription of CYP1A1 gene. Diyerin increases CYP1A1 gene transcription and activity, inhibits CYP1A1 enzyme activity, thereby inhibiting the activation of carcinogens.
Dioxynignin can inhibit the proliferation of MCF-7 cells and promote cell apoptosis by activating the JNK cell apoptosis pathway in vitro. Dioxynignin inhibited the proliferation of breast cancer MDA-MB468 and normal breast MCF-10a cells. It was found that this compound is selective for cancer cells, slightly toxic to normal breast cells, and makes MDA-MB468 cells arrest in the G1 phase. lag. Diyerin, extracted from traditional Chinese medicine, has been found to have anticancer activity.
Nervous system disease
Oral administration of diosmin reduces levels of brain β-amyloid (Aβ) oligomers and increases inhibitory glycogen synthase in a mouse model of tau hyperphosphorylation and cognitive impairment in Alzheimer’s disease (AD) Kinase 3 (GSK-3β) phosphorylation while selectively reducing γ-secretase activity, Aβ denaturation, tau hyperphosphorylation, and pro-inflammatory effects in microglia in vitro. Therefore, diosmin is considered to have a therapeutic effect on AD.
Dioxynignin can protect retinal cell damage induced by doxorubicin (ADR), effectively reduce ADR-mediated inhibition of proliferation and apoptosis in SD rats and human retinal pigment epithelial cells (ARPE-19). Diyerin inhibited ADR-induced oxidative stress, DNA damage, and mitochondrial damage in ARPE-19, decreased ROS levels, increased intracellular GDH levels, and significantly reversed the expression of Bcl-2 protein in ARPE-19 cells induced by ADR. Therefore, diosmin can protect eyesight by reducing DNA damage and reducing apoptosis caused by oxidative stress in ARPE-19 cells through anti-oxidation.
In citrus fruits, diosmin has anti-inflammatory and antioxidant properties. In a mouse model of bombesin-induced acute pancreatitis (AP), diosmin pretreatment significantly reduced serum amylase and lipase levels, histological damage, tumor necrosis factor (TNF-α) secretion, Interleukin (IL) 1β, IL-6, myeloperoxidase (MPO) activity, trypsinogen activating peptide (TAP) level, induced expression of nitric oxide synthase (iNOS), and activated NF-κB signaling pathway. Therefore, diosmin may become a new therapeutic drug in future clinical trials for the treatment of AP. In vitro, diosmin scavenge free radicals. Therefore, by inhibiting NF-κB signaling through antioxidative effects, reducing inflammatory mediators and cytokines, and inhibiting hepatocyte apoptosis, diosmin has protective effects against endotoxin-induced acute liver failure in mice.
Acute lung injury (ALI)/acute respiratory distress syndrome (ARDS) is a common clinical syndrome of diffuse pneumonia with high mortality and limited treatment options. Due to its antioxidant and anti-inflammatory effects, diosmin has long been considered as an active ingredient in Chinese herbal medicine. In human bronchial epithelial cells (HBE), transforming growth factor-β1 (TGF-β1) enhanced EMT and ROS production, and diosmin significantly inhibited TGF-β1-induced increased cell migration and N-cadherin calcium, cadherin, Alterations in muscle actin expression. In addition, diosmin inhibited TGF-β1-induced intracellular ROS generation, PI3K/Akt and MAPK pathways, down-regulated NOX4, and up-regulated the expressions of SOD and catalase. It was demonstrated that diosmin attenuated TGF-β1-induced EMT by inhibiting ROS generation and inactivating PI3K/Akt and MAPK pathways to reduce the process of airway remodeling and fibrosis.
Through anti-inflammation, anti-oxidation and triggering different signaling pathways, diosmin can reduce lung histopathological changes and alleviate respiratory diseases such as EMT, bronchial asthma and lung injury.